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Table 2 Results of the preliminary screening of nipecotic acid bioisosteres as GAT inhibitors by Sowa [113]

From: Visualizing GABA transporters in vivo: an overview of reported radioligands and future directions

Compound

Inhibition (%)

Normalized to tiagabine

− 3

− 10.7

− 4

− 14.3

4

14.3

9

32.1

− 6

− 21.4

Tiagabine

28

100

  1. Inhibition was measured using [3H]GABA uptake inhibition assay in rat brain homogenate